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1. 发明申请

WO2004074270A2 INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME 审中-公开
标题翻译： HEPATITIS C病毒RNA依赖RNA聚合酶的抑制剂及其组合物和治疗
公开(公告)号：WO2004074270A2
公开(公告)日：2004-09-02
申请号：PCT/IB2004000493
申请日：2004-02-09
申请人： PFIZER , BORCHARDT ALLEN JOHN , GONZALEZ JAVIER , LI HUI , LINTON MARIA ANGELICA , TATLOCK JOHN HOWARD
发明人： BORCHARDT ALLEN JOHN , GONZALEZ JAVIER , LI HUI , LINTON MARIA ANGELICA , TATLOCK JOHN HOWARD
IPC分类号： A61K31/4025 , A61K31/452 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P31/14 , C07D263/58 , C07D285/06 , C07D309/32 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/06 , C07D407/10 , C07D407/12 , C07D409/06 , C07D409/10 , C07D413/02 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/02 , C07D417/06 , C07D417/10 , C07D417/12 , C07D471/04 , C07D473/30 , C07D473/36 , C07D487/04 , C07D495/04 , C07D513/04 , A61K31/351
CPC分类号： C07D285/06 , C07D263/58 , C07D309/32 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/06 , C07D407/10 , C07D407/12 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/10 , C07D417/12 , C07D471/04 , C07D473/30 , C07D473/36 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The invention relates to compounds of the formula (I) and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R and R , are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula (I), and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula (I). The invention also relates to methods of preparing the compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，溶剂合物，前药和代谢物，其中W，Z，R 1和R 2如本文所定义。本发明还涉及通过施用式（I）化合物和用于治疗含有式（I）化合物的这种病症的药物组合物来治疗哺乳动物中的丙型肝炎病毒的方法。本发明还涉及制备式（I）化合物的方法。

2. 发明申请

WO02055521A1 PURINE DERIVATIVES AS PURINERGIC RECEPTOR ANTAGONISTS 审中-公开
标题翻译：嘌呤衍生物作为纯化受体拮抗剂
公开(公告)号：WO02055521A1
公开(公告)日：2002-07-18
申请号：PCT/GB2002/000076
申请日：2002-01-10
IPC分类号： A61K31/198 , A61K31/52 , A61K31/695 , A61K45/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D473/00 , C07D473/28 , C07D473/32 , C07D473/36 , C07D473/40
CPC分类号： C07D473/00 , A61K31/52 , C07D473/28 , C07D473/32 , C07D473/36 , C07D473/40
摘要： Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3 is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11 and SO2R11; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an (NR5R6) group then R5 and R6 may be linked to form a heterocyclic ring; R7 is selected from alkyl and aryl; R8, R9 and R10 are independently selected from H, alkyl and aryl, or R9 and R10 may be linked to form a heterocyclic ring, or where R8, R9 and R10 are in a (CONR8NR9R10) group, R8 and R9 may be linked to form a heterocyclic group; and R11 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.
摘要翻译：其中R1选自烷基，芳基，烷氧基，芳氧基，硫代烷基，硫代芳基，CN，卤素，NR5R6，NR4COR5，NR4CONR5R6，NR4CO2R7和NR4SO2R7的式（Ⅰ）化合物; R2选自含N，O或S的杂芳基，其中所述杂芳基通过不饱和碳原子连接，所述不饱和碳原子与一个或两个N，O或S-杂原子相邻，邻近邻二取代杂芳基; R3选自H，烷基，COR8，CONR9R10，CONR8NR9R10，CO2R11和SO2R11; R 4，R 5和R 6独立地选自H，烷基和芳基，或其中R 5和R 6在（NR 5 R 6）基团中，则R 5和R 6可以连接形成杂环; R7选自烷基和芳基; R 8，R 9和R 10独立地选自H，烷基和芳基，或R 9和R 10可以连接形成杂环，或其中R8，R9和R10在（CONR8NR9R10）基团中，R8和R9可以连接到形成杂环基; R 11选自烷基和芳基，或其药学上可接受的盐或前药，用于治疗或预防嘌呤受体，特别是腺苷受体，特别是A 2A受体的阻断可能是有益的病症，特别是其中所述障碍是运动障碍，例如帕金森病或所述障碍是抑郁症，认知障碍或记忆障碍，急性或慢性疼痛，ADHD或发作性睡病，或对受试者的神经保护; 用于治疗的式（I）化合物; 和式（I）的新化合物本身。

3. 发明申请

WO2015164573A1 PURINE DERIVATIVES AS CD73 INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：作为CD73抑制剂治疗癌症的嘌呤衍生物
公开(公告)号：WO2015164573A1
公开(公告)日：2015-10-29
申请号：PCT/US2015/027235
申请日：2015-04-23
申请人： VITAE PHARMACEUTICALS, INC.
发明人： CACATIAN, Salvacion , CLAREMON, David A. , JIA, Lanqi , MORALES-RAMOS, Angel , SINGH, Suresh B. , VENKATRAMAN, Shankar , XU, Zhenrong , ZHENG, Yajun
IPC分类号： C07D473/40 , C07D473/34 , C07D473/36 , C07D405/04 , C07H19/06 , C07H19/16 , A61K31/506 , A61K31/675 , A61K31/7052 , A61P33/00
CPC分类号： C07H19/16 , A61K31/517 , A61K31/675 , A61K31/7056 , A61K31/7072 , A61K31/7076 , A61K45/06 , C07D239/72 , C07D405/04 , C07D473/34 , C07D473/36 , C07D473/40 , C07F9/65128 , C07F9/65616 , C07H19/052 , C07H19/06
摘要： Provided are novel compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are inhibitors of CD73 and are useful in the treatment of cancer.
摘要翻译：提供了新的化合物，其药学上可接受的盐及其药物组合物，其是CD73的抑制剂并且可用于治疗癌症。

4. 发明申请

WO2009006431A2 BIOLOGICALLY ACTIVE APHROCALLISTIN COMPOUNDS 审中-公开
标题翻译：生物活性APHROCALLISTIN化合物
公开(公告)号：WO2009006431A2
公开(公告)日：2009-01-08
申请号：PCT/US2008/068834
申请日：2008-06-30
申请人： FLORIDA ATLANTIC UNIVERSITY BOARD OF TRUSTEES , WRIGHT, Amy, E. , SENNETT, Susan, H. , POMPONI, Shirley, A. , MCCARTHY, Peter, J. , GUZMAN, Esther, A.
发明人： WRIGHT, Amy, E. , SENNETT, Susan, H. , POMPONI, Shirley, A. , MCCARTHY, Peter, J. , GUZMAN, Esther, A.
IPC分类号： A61K31/335 , A61K31/16 , A61K31/40
CPC分类号： C07D473/34 , C07D473/30 , C07D473/36
摘要： The subject invention provides novel compositions of biologically active compounds which can advantageously be used in blocking cellular proliferation and/or treatment of cancer.
摘要翻译：本发明提供了可有利地用于阻断细胞增殖和/或治疗癌症的生物活性化合物的新组合物。

5. 发明申请

WO2004074270B1 INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME 审中-公开
标题翻译： HEPATITIS C病毒RNA依赖RNA聚合酶的抑制剂及其组合物和治疗
公开(公告)号：WO2004074270B1
公开(公告)日：2005-03-17
申请号：PCT/IB2004000493
申请日：2004-02-09
申请人： PFIZER , BORCHARDT ALLEN JOHN , GONZALEZ JAVIER , LI HUI , LINTON MARIA ANGELICA , TATLOCK JOHN HOWARD
发明人： BORCHARDT ALLEN JOHN , GONZALEZ JAVIER , LI HUI , LINTON MARIA ANGELICA , TATLOCK JOHN HOWARD
IPC分类号： A61K31/4025 , A61K31/452 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P31/14 , C07D263/58 , C07D285/06 , C07D309/32 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/06 , C07D407/10 , C07D407/12 , C07D409/06 , C07D409/10 , C07D413/02 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/02 , C07D417/06 , C07D417/10 , C07D417/12 , C07D471/04 , C07D473/30 , C07D473/36 , C07D487/04 , C07D495/04 , C07D513/04 , A61K31/351
CPC分类号： C07D285/06 , C07D263/58 , C07D309/32 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/06 , C07D407/10 , C07D407/12 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/10 , C07D417/12 , C07D471/04 , C07D473/30 , C07D473/36 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The invention relates to compounds of the formula (I) and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R and R , are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula (I), and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula (I). The invention also relates to methods of preparing the compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，溶剂合物，前药和代谢物，其中W，Z，R 1和R 2如本文所定义。本发明还涉及通过施用式（I）化合物和用于治疗含有式（I）化合物的这种病症的药物组合物来治疗哺乳动物中的丙型肝炎病毒的方法。本发明还涉及制备式（I）化合物的方法。

6. 发明申请

WO2008150364A1 CYCLOPROPYL PYRROLIDINE OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：环丙基吡咯烷OREXIN受体拮抗剂
公开(公告)号：WO2008150364A1
公开(公告)日：2008-12-11
申请号：PCT/US2008/006396
申请日：2008-05-19
申请人： MERCK & CO., INC. , COLEMAN, Paul, J. , MERCER, Swati, P. , ROECKER, Anthony, J.
发明人： COLEMAN, Paul, J. , MERCER, Swati, P. , ROECKER, Anthony, J.
IPC分类号： A01N43/82 , A01N43/78 , A61K31/41
CPC分类号： C07D417/14 , A61K31/401 , A61K31/4015 , A61K31/403 , A61K31/41 , C07D403/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/06 , C07D473/36 , C07D498/04
摘要： The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体的拮抗剂的环丙基脯氨酸双酰胺化合物，其可用于治疗或预防涉及食欲肽受体的神经和精神病症和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

7. 发明申请

WO0051993A3 DIHETERO-SUBSTITUTED METALLOPROTEASE INHIBITORS 审中-公开
标题翻译： DIHETERO取代的金属蛋白酶抑制剂
公开(公告)号：WO0051993A3
公开(公告)日：2000-12-21
申请号：PCT/US0005195
申请日：2000-03-01
申请人： PROCTER & GAMBLE
发明人： CHENG MENYAN , ALMSTEAD NEIL GREGORY , NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , DE BISWANATH
IPC分类号： C07C311/29 , C07C317/48 , C07D213/65 , C07D213/70 , C07D233/84 , C07D235/28 , C07D239/95 , C07D249/10 , C07D257/04 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/36 , C07D277/74 , C07D285/08 , C07D307/38 , C07D311/16 , C07D333/34 , C07D413/04 , C07D473/36
CPC分类号： C07D213/70 , C07C311/29 , C07C317/48 , C07C323/58 , C07D213/65 , C07D233/84 , C07D235/28 , C07D239/95 , C07D249/10 , C07D257/04 , C07D263/58 , C07D271/113 , C07D277/74 , C07D285/08 , C07D307/38 , C07D311/16 , C07D333/34 , C07D413/04 , C07D473/36
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to formula (I): where J, M, Q, T, W, X, Z, R , R , R , R , R , R , R , R , R , m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
摘要翻译：公开了作为金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。特别地，化合物具有式（I）的结构：其中J，M，Q，T，W，X，Z，R 1，R 2，R 3，R 4， R 4，R 5，R 6，R 6'，R 7，m和n具有说明书中描述的含义。本发明还包括上式的光学异构体，非对映异构体和对映异构体及其药学上可接受的盐，可生物水解的酰胺，酯和酰亚胺。还公开了包含这些化合物的药物组合物，以及使用该化合物或药物组合物治疗或预防金属蛋白酶相关疾病的方法。

8. 发明申请

WO00051993A2 DIHETERO-SUBSTITUTED METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：二取代的金属蛋白酶抑制剂
公开(公告)号：WO00051993A2
公开(公告)日：2000-09-08
申请号：PCT/US2000/005195
申请日：2000-03-01
IPC分类号： C07C311/29 , C07C317/48 , C07D213/65 , C07D213/70 , C07D233/84 , C07D235/28 , C07D239/95 , C07D249/10 , C07D257/04 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/36 , C07D277/74 , C07D285/08 , C07D307/38 , C07D311/16 , C07D333/34 , C07D413/04 , C07D473/36 , C07D277/00
CPC分类号： C07D213/70 , C07C311/29 , C07C317/48 , C07C323/58 , C07D213/65 , C07D233/84 , C07D235/28 , C07D239/95 , C07D249/10 , C07D257/04 , C07D263/58 , C07D271/113 , C07D277/74 , C07D285/08 , C07D307/38 , C07D311/16 , C07D333/34 , C07D413/04 , C07D473/36
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to formula (I): where J, M, Q, T, W, X, Z, R , R , R , R , R , R , R , R , R , m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
摘要翻译：本发明涉及适用于治疗以这些酶的过度活性为特征的病症的金属蛋白酶抑制化合物。更具体地说，这些化合物具有根据通式（I）的结构。在该通式（I）中，J，M，Q，T，W，X，Z，R 1，R 2，R 3，R 4，R 4'，R R 5，R 6，R 6'，R 7，m和n具有由说明书给出的含义。本发明还涉及该式的光学异构体，非对映异构体，对映异构体以及它们的一些药学上可接受的盐，生物可水解的酰胺，酯和酰亚胺。本发明一方面还涉及包含这些化合物的药物组合物，另一方面涉及使用这些化合物的程序以及涉及这些药物组合物用于治疗或预防涉及金属蛋白酶的疾病的方法。

9. 发明申请

WO2009081105A2 QUINOXALINE AND QUINOLINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：喹诺酮和喹啉衍生物作为激酶抑制剂
公开(公告)号：WO2009081105A2
公开(公告)日：2009-07-02
申请号：PCT/GB2008004171
申请日：2008-12-17
申请人： UCB PHARMA SA , ALLEN DANIEL REES , BUCKLEY GEORGE MARTIN , BUERLI ROLAND , DAVENPORT RICHARD JOHN , KINSELLA NATASHA , LOCK CHRISTOPHER JAMES , LOWE CHRISTOPHER , MACK STEPHEN ROBERT , PITT WILLIAM ROSS , RATCLIFFE ANDREW JAMES , RICHARD MARIANNA DILANI , SABIN VERITY MARGARET , SHARPE ANDREW , TAIT LAURA JANE , WARRELOW GRAHAM JOHN , WILLIAMS SOPHIE CAROLINE
发明人： ALLEN DANIEL REES , BUCKLEY GEORGE MARTIN , BUERLI ROLAND , DAVENPORT RICHARD JOHN , KINSELLA NATASHA , LOCK CHRISTOPHER JAMES , LOWE CHRISTOPHER , MACK STEPHEN ROBERT , PITT WILLIAM ROSS , RATCLIFFE ANDREW JAMES , RICHARD MARIANNA DILANI , SABIN VERITY MARGARET , SHARPE ANDREW , TAIT LAURA JANE , WARRELOW GRAHAM JOHN , WILLIAMS SOPHIE CAROLINE
IPC分类号： C07D401/14 , A61K31/395 , A61P35/00 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36
CPC分类号： C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36
摘要： A series of heteroaryl-substituted quinoxaline and quinoline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译：因此，作为PI3激酶的选择性抑制剂的一系列杂芳基取代的喹喔啉和喹啉衍生物在医学中是有益的，例如在治疗炎症，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害感受性或眼科疾病中。

10. 发明申请

WO2009006431A3 BIOLOGICALLY ACTIVE APHROCALLISTIN COMPOUNDS 审中-公开
标题翻译：生物活性花青素化合物
公开(公告)号：WO2009006431A3
公开(公告)日：2009-03-05
申请号：PCT/US2008068834
申请日：2008-06-30
申请人： FLORIDA ATLANTIC UNIVERSITY BO , WRIGHT AMY E , SENNETT SUSAN H , POMPONI SHIRLEY A , MCCARTHY PETER J , GUZMAN ESTHER A
发明人： WRIGHT AMY E , SENNETT SUSAN H , POMPONI SHIRLEY A , MCCARTHY PETER J , GUZMAN ESTHER A
IPC分类号： A61K31/335 , A61K31/165 , A61K31/40 , C07D305/14
CPC分类号： C07D473/34 , C07D473/30 , C07D473/36
摘要： The subject invention provides novel compositions of biologically active compounds which can advantageously be used in blocking cellular proliferation and/or treatment of cancer.
摘要翻译：本发明提供了可有利地用于阻断癌细胞增殖和/或治疗的生物活性化合物的新组合物。

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